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报道与α１－受体拮抗剂ＤＤＰＨ相关的芳氧烷胺类去手性碳类似物４ａ～４ｉ，Ｎ－甲基化类似物５ａ～５ｊ，６及构象限制化合物８～１２的设计、合成和降压活性。目的物及酰胺中间体的结构经元素分析，红外光谱，核磁共振氢谱和质谱数据确证。药理实验结果表明，去手性碳类似物的降压活性一般优于相应的同位手性碳、异位手性碳及构象限制化合物；在Ｎ－原子上引入甲基可提高化合物的降压活性（４ｈ／５ｊ）；５ｊ和ＤＤＰＨ的活性对比表明５ｊ的活性优于ＤＤＰＨ。
Reported the design, synthesis, and synthesis of the aryloalkanamine deacetylated carbon analogs 4a-4i, N-methylated analogs 5a-5j, 6 and conformational-restricted compounds 8-12 related to the α1-receptor antagonist DDPH Antihypertensive activity. The structures of the target compounds and amide intermediates were confirmed by elemental analysis, IR, 1H-NMR and MS data. Pharmacological results show that the antihypertensive activity of the chiral carbon analogues is generally better than that of the corresponding isomeric chiral carbons, the ectopic chiral carbons and the conformational limiting compounds. The introduction of methyl groups on the N-atom enhances the antihypertensive activity of the compounds (4h / 5j); 5j and DDPH activity comparison shows that the activity of 5j better than DDPH.